Drug solubility in phospholipid carrier as a predictive parameter for drug recovery in microparticles produced by the aerosol solvent extraction system (ASES) process

Abstract

The solubility of various drugs in a constant ratio of phosphatidylcholine- cholesterol carrier were studied to investigate their influence on drug recovery in drug-lipid microparticles produced by the aerosol solvent extraction system (ASES) process. Solubility of the drugs in such lipid carrier were determined by using differential scanning calorimetry and confirmed by X-ray powder diffraction study. The results showed that drug possessing relatively high solubility in the lipid carrier used could lead to a higher amount of drug recovered in the drug-lipid microparticles produced. However, too high amount of dissolved drug imposed an adverse effect on the solidification of the lipid carrier during ASES processing, which led to partial film formation in the production column and hence a lower yield of microparticles. Such adverse effect was not the case for the drugs with low solubility in the carrier but there was an incomplete recovery of drug in the produced microparticles due to the partial extraction by the supercritical gas instead. The maximum amount of drug recovered in the ASES-prepared microparticles was found to correlate to the solubility of drug in the lipid carrier so that it might be utilized as a predictive parameter for determining the amount of drug to be incorporated into the microparticles. Copyright © Informa Healthcare USA, Inc.